scholarly journals Preparation and in vitro characterization of gellan based floating beads of acetohydroxamic acid for eradication of H. pylori

2007 ◽  
Vol 57 (4) ◽  
pp. 413-427 ◽  
Author(s):  
Parauvathanahalli Rajinikanth ◽  
Brahmeshwar mishra
Keyword(s):  
Drug Release ◽  
Encapsulation Efficiency ◽  
Diffusion Mechanism ◽  
Oral Dosage ◽  
Acetohydroxamic Acid ◽  
Burst Release ◽  
Sustained Drug Release ◽  
H Pylori

Preparation andin vitrocharacterization of gellan based floating beads of acetohydroxamic acid for eradication ofH. pyloriGellan based floating beads of acetohydroxamic acid (AHA) were prepared by the ionotropic gellation method to achieve controlled and sustained drug release for treatment ofHelicobacter pyloriinfection. The prepared beads were evaluated for diameter, surface morphology and encapsulation efficiency. Formulation parameters like concentrations of gellan, chitosan, calcium carbonate and the drug influenced thein vitrodrug release characteristics of beads. Drug and polymer interaction studies were carried out using differential scanning calorimetry. Chitosan coating increased encapsulation efficiency of the beads and reduced the initial burst release of the drug from the beads. Kinetic treatment of the drug release data revealed a matrix diffusion mechanism. Prepared floating beads showed good antimicrobial activity (in vitro H. pyloriculture) as potent urease inhibitors. In conclusion, an oral dosage form of floating gellan beads containing AHA may form a useful stomach site specific drug delivery system for the treatment ofH. pyloriinfection.

scholarly journals Preparation and Evaluation of Intraperitoneal Long-Acting Oxaliplatin-Loaded Multi-Vesicular Liposomal Depot for Colorectal Cancer Treatment

Pharmaceutics ◽  
2020 ◽  
Vol 12 (8) ◽  
pp. 736
Author(s):  
Sharif Md Abuzar ◽  
Eun Jung Park ◽  
Yeji Seo ◽  
Juseung Lee ◽  
Seung Hyuk Baik ◽  
...  
Keyword(s):  
Colorectal Cancer ◽  
Drug Release ◽  
Entrapment Efficiency ◽  
Lag Phase ◽  
Burst Release ◽  
Sustained Drug Release ◽  
Long Acting ◽  
High Entrapment Efficiency

Colorectal cancer with peritoneal metastasis has a poor prognosis because of inadequate responses to systemic chemotherapy. Cytoreductive surgery followed by intraperitoneal (IP) chemotherapy using oxaliplatin has attracted attention; however, the short half-life of oxaliplatin and its rapid clearance from the peritoneal cavity limit its clinical application. Here, a multivesicular liposomal (MVL) depot of oxaliplatin was prepared for IP administration, with an expected prolonged effect. After optimization, a combination of phospholipids, cholesterol, and triolein was used based on its ability to produce MVL depots of monomodal size distribution (1–20 µm; span 1.99) with high entrapment efficiency (EE) (92.16% ± 2.17%). An initial burst release followed by a long lag phase of drug release was observed for the MVL depots system in vitro. An in vivo pharmacokinetic study mimicking the early postoperative IP chemotherapy regimen in rats showed significantly improved bioavailability, and the mean residence time of oxaliplatin after IP administration revealed that slow and continuous erosion of the MVL particles yielded a sustained drug release. Thus, oxaliplatin-loaded MVL depots presented in this study have potential for use in the treatment of colorectal cancer.

scholarly journals Design and characterization of chitosan-containing mucoadhesive buccal patches of propranolol hydrochloride

2007 ◽  
Vol 57 (1) ◽  
pp. 61-72 ◽  
Author(s):  
Vishnu Patel ◽  
Bhupendra Prajapati ◽  
Madhabhai Patel
Keyword(s):  
Drug Release ◽  
Ex Vivo ◽  
Stability Study ◽  
Fickian Diffusion ◽  
Content Uniformity ◽  
Propranolol Hydrochloride ◽  
Sustained Drug Release ◽  
Surface Ph

Design and characterization of chitosan-containing mucoadhesive buccal patches of propranolol hydrochloride Mucoadhesive buccal patches containing propranolol hydrochloride were prepared using the solvent casting method. Chitosan was used as bioadhesive polymer and different ratios of chitosan to PVP K-30 were used. The patches were evaluated for their physical characteristics like mass variation, drug content uniformity, folding endurance, ex vivo mucoadhesion strength, ex vivo mucoadhesion time, surface pH, in vitro drug release, and in vitro buccal permeation study. Patches exhibited controlled release for a period of 7 h. The mechanism of drug release was found to be non-Fickian diffusion and followed the first-order kinetics. Incorporation of PVP K-30 generally enhanced the release rate. Swelling index was proportional to the concentration of PVP K-30. Optimized patches (F4) showed satisfactory bioadhesive strength of 9.6 ± 2.0 g, and ex vivo mucoadhesion time of 272 minutes. The surface pH of all patches was between 5.7 and 6.3 and hence patches should not cause irritation in the buccal cavity. Patches containing 10 mg of drug had higher bioadhesive strength with sustained drug release as compared to patches containing 20 mg of drug. Good correlation was observed between the in vitro drug release and in vitro drug permeation with a correlation coefficient of 0.9364. Stability study of optimized patches was done in human saliva and it was found that both drug and buccal patches were stable.

scholarly journals Preparation and Biological Evaluation of Silybin Liposomes for the Treatment of Liver Disorders

2021 ◽  
pp. 186-200
Author(s):  
Saijyosthana Gandey ◽  
Vema Aparna ◽  
Raghupathi Kandarapu
Keyword(s):  
Drug Release ◽  
Phosphatidyl Choline ◽  
Animal Studies ◽  
Encapsulation Efficiency ◽  
In Vitro Release ◽  
Biological Evaluation ◽  
Sustained Drug Release ◽  
Vesicle Size

Aim: The aim of the present study was to develop silybin liposome by incorporating phosphatidyl choline & cholesterol so as to increase its oral bioavailability and liver targeted enhanced hepatoprotection. Methodology: Thin film hydration technique was used for the development of liposomes by using phosphatidyl choline, cholesterol and drug. Liposomes were evaluated for vesicle size, zeta potential, PDI, encapsulation efficiency, surface morphology and in vitro drug release study. Further the optimized formulation was evaluated for APAP-induced alterations in liver and kidney function tests in rats and histopathological studies. Results: The results were promising with a sustained drug release of 80% within 20hrs, optimized vesicle size of 276nm and 89% encapsulation efficiency. The animal studies demonstrated superior hepatoprotective effect compared to silybin solution. Conclusion: The silybin liposomes showed better in-vitro release & in-vivo hepatoprotection along with better animal activity & improvement in histopathological changes as compared to silybin.

In vitro drug release and antibacterial activity evaluation of silk fibroin coated vancomycin hydrochloride loaded poly (lactic-co-glycolic acid) (PLGA) sustained release microspheres

2022 ◽  
pp. 088532822110640
Author(s):  
Shengtang Li ◽  
Xuewen Shi ◽  
Bo Xu ◽  
Jian Wang ◽  
Peng Li ◽  
...  
Keyword(s):  
Drug Release ◽  
Encapsulation Efficiency ◽  
Glycolic Acid ◽  
Drug Loading ◽  
Burst Release ◽  
Plga Microspheres ◽  
In Vitro Drug Release ◽  
Initial Burst ◽  
Initial Burst Release

Currently, the treatment of osteomyelitis poses a great challenge to clinical orthopedics. The use of biodegradable materials combined with antibiotics provides a completely new option for the treatment of osteomyelitis. In this study, vancomycin hydrochloride (VANCO) loaded poly (lactic-co-glycolic acid) (PLGA) microspheres were prepared by a double emulsion solvent evaporation method, and the in vitro drug release behaviors of the drug loaded microspheres were explored after coating with different concentrations of silk fibroin (SF). Drug loading, encapsulation efficiency, Scanning electron microscopy, particle size analysis, Fourier transform infrared spectroscopy, hydrophilicity, in vitro drug release, and in vitro antibacterial activity were evaluated. The results showed that the drug loading of vancomycin loaded PLGA microspheres was (24.11 ±1.72)%, and the encapsulation efficiency was (48.21 ±3.44)%. The in vitro drug release indicated that the drug loaded microspheres showed an obvious initial burst release, and the drug loaded microspheres coated with SF could alleviate the initial burst release in varying degrees. It also can reduce the amount of cumulative drug release, and the effect of microspheres coated with 0.1% concentration of SF is the best. The time of in vitro drug release in different groups of drug loaded microspheres can be up to 28 days. The microspheres coated with (0.1%SF) or without (0%SF) SF showed a cumulative release of (82.50±3.51)% and (67.70±3.81)%,respectively. Therefore, the surface coating with SF of vancomycin loaded microspheres can alleviate the initial burst release, reduce the cumulative drug release, potentially prolong the drug action time, and improve the anti-infection effect.

Controlled Release of Naproxen Sodium from Eudragit RS 100 Transdermal Film

1970 ◽  
Vol 3 (1) ◽  
Author(s):  
Masuda Khatun ◽  
SM Ashraful Islam ◽  
Parvin Akter ◽  
Mohiuddin Abdul Quadir ◽  
Md. Selim Reza
Keyword(s):  
Controlled Release ◽  
Drug Release ◽  
Naproxen Sodium ◽  
Diffusion Mechanism ◽  
Active Principle ◽  
Burst Release ◽  
Drug Load ◽  
Eudragit Rs ◽  
Peg 4000

Polymeric films of Eudragit RS 100 were prepared by solvent casting method to explore the possibilities of using this polymer in transdermal therapeutic system (TTS). Naproxen was used as a model drug and incorporated in two different percent loading (8.3 % w/w and 20.8 % w/w of films). Effects of two plasticizers ( PEG 1500 and PEG 4000) and two release modifiers ( PVA and HPMC 15cps) on in vitro drug release from naproxen loaded eudragit RS films were assessed. Drug release was found to be a function of drug load, PEG molecular weight and physico-chemical property of the release modifiers incorporated. At low drug load, highest amount of drug was released from flims containing PEG 1500 (more than 95%). However, a burst release was evident in case of all the experimental batches except that loaded with HPMC 15 cps. With this formulation, more than 75 % of active principle was released after 8 hours while only 12 % of naproxen was liberated in the first hour of dissolution. Increasing drug load, increased the rate and extent of drug release from eudragit RS films; however this effect was minimized when PEG 4000 was used as release modifier. For PEG 1500 loaded films, drug release was decreased with increasing drug concentration in the TTS. Inclusion of PEG in eudragit RS films caused the drug to be released by diffusion (Fickian) kinetics whereas PVA and HPMC containing formulations released drug by diffusion mechanism coupled with erosion. Key words: Naproxen sodium, Eudragit RS 100, Controlled release. Dhaka Univ. J. Pharm. Sci. Vol.3(1-2) 2004 The full text is of this article is available at the Dhaka Univ. J. Pharm. Sci. website

scholarly journals Formulation development and characterization of eplerenone insitu oralgels

2021 ◽  
pp. 69-78
Author(s):  
M.Parthy ◽  
T.Malyadri ◽  
Ch.Saibabu
Keyword(s):  
Drug Release ◽  
Oral Dosage ◽  
Gelling Agent ◽  
In Vitro Dissolution ◽  
Compatibility Study ◽  
Gastric Retention ◽  
Formulation Development ◽  
Sustained Drug Release

Gastro retentive drug delivery systems have been widely used to prolong the retention of dosage forms in the stomach. Among the various approaches, the floating in-situ gelling formulation offers sustained drug release as well as prolonged gastric retention, along with the added advantage of the liquid oral dosage form. The present study was an attempt to formulate and evaluate floating in situ gel of Eplerenone by using various polymers like Xanthan gum, Carbopol, HPMC K100M, and Karaya gum which undergoes pH dependant sol-gel transition at gastric pH, thereby prolonging the retention of the system in the stomach. Sodium alginate a natural polymer was employed as a gelling agent where Gelation is triggered by the source of calcium ions in the form of calcium carbonate. Drug and polymers were subjected for compatibility study using FTIR studies, which revealed that there was no interaction between drugs and polymers. The evaluation was carried out for invitro parameters such as gelling nature, Total floating time, drug content, viscosity, & in vitro dissolution studies. Among all the formulations, the F12 formulation containing HPMC K100M was chosen as an optimized formulation that shows maximum drug release by the end of 12hrs and has excellent floating characteristics and gastric retention. From kinetic studies, the optimized formulation shows zero-order release with super case II transport mechanism.

scholarly journals Fabrication and Characterization of Ceftizoxime-Loaded Pectin Nanocarriers

Nanomaterials ◽  
2020 ◽  
Vol 10 (8) ◽  
pp. 1452
Author(s):  
Pawan Kumar ◽  
Vinod Kumar ◽  
Ravinder Kumar ◽  
Catalin Iulian Pruncu
Keyword(s):  
Drug Release ◽  
Bacterial Infections ◽  
Enterobacter Aerogenes ◽  
Sustained Drug Release ◽  
In Vitro Drug Release ◽  
Method Optimization ◽  
Dialysis Method ◽  
Nose And Throat

Ceftizoxime (C13H12N5NaO5S2) is a parenteral, third-generationcephalosporin antibiotic used to treat bacterial infections including ear, nose, and throat infections. In this work, pectin has been used as a nanocarrier for ceftizoxime due to its high biocompatibility and non-toxicity with tunable surface properties. Ceftizoxime-loaded pectin nanocarriers (CPN) were successfully synthesized by the solvent displacement method. Optimization of nanoformulation was done by response surface methodology using Design-Expert software. The optimized formulation examined various in-vitro characterizations such as particle size, morphology, and FTIR studies. TEM results revealed irregular shape nanoparticles within the range of 29–110 nm. The in-vitro drug release using the dialysis method was performed after 24 h where nanoformulation showed sustained drug release. Drug-loaded nanoparticles revealed good antimicrobial activity against Bacillus cereus, Bacillus polymyxa, Enterobacter aerogenes, and Pseudomonas aeruginosa.

scholarly journals Formulation and Invitro characterization of Flurbiprofen loaded Nanosponges

2021 ◽  
Vol 12 (3) ◽  
pp. 1798-1802
Author(s):  
Gangadhara R. ◽  
Satheesh K. P. ◽  
Devanna N. ◽  
Sasikala L. ◽  
Vandavasi Koteswara Rao
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Guar Gum ◽  
Entrapment Efficiency ◽  
Sustained Drug Release ◽  
In Vitro Drug Release ◽  
Topical Gel ◽  
High Entrapment Efficiency

The aim of this analysis is to see how effective a Nanosponge-loaded topical gel is at distributing flurbiprofen through the skin. Flurbiprofen was entrapped in Nanosponge and formulated into a gel for this purpose. Flurbiprofen Nanosponges were developed by solvent evaporation using pluronic F68 and ethyl cellulose. The particle size and entrapment quality were discovered to be in the range of 200-410 nm and 90.94% to 98.68%, respectively. For gel formulation, Nanopsonges with high entrapment efficiency and the smallest particle size (F3) were chosen based on the characterization. Using Guar gum, Carbopol, and HPMC K4M, a total of 6 formulations were produced to determine the sustained drug release and were tested for physiochemical tests, producing positive results. According to the findings of the above in vitro drug release trials, formulations containing carbopol release more drug at the end of 11 hours than other formulations and follow a zero-order with case II transport mechanism.

scholarly journals Chitosan-Modified PLGA Nanoparticles for Control-Released Drug Delivery

Polymers ◽  
2019 ◽  
Vol 11 (2) ◽  
pp. 304 ◽  
Author(s):  
Boting Lu ◽  
Xikun Lv ◽  
Yuan Le
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Encapsulation Efficiency ◽  
Packed Bed ◽  
Plga Nanoparticles ◽  
Burst Release ◽  
Sustained Drug Release ◽  
Drug Delivery Carrier ◽  
Rotating Packed Bed ◽  
Drug Encapsulation Efficiency

Poly (lactic-co-glycolic acid) nanoparticles (PLGA NPs) are well recognized as an ideal drug delivery carrier for their biocompatibility and biodegradability. In order to overcome the disadvantage of drug burst release, chitosan (CS) was used to modify the PLGA nanoparticles. In this work, CS-PLGA nanoparticles with different ratio of CS to PLGA were prepared using high-gravity rotating packed bed (RPB). With the increase of amount of CS, the particle size increased from 132.8 ± 1.5 nm to 172.7 ± 3.2 nm, zeta potential increased from −20.8 ± 1.1 mV to 25.6 ± 0.6 mV, and drug encapsulation efficiency increased from 65.8% to 87.1%. The initial burst release of PLGA NPs reduced after being modified by CS, and the cumulative release was 66.9%, 41.9%, 23.8%, and 14.3%, after 2 h, respectively. The drug release of CS-modified PLGA NPs was faster at pH5.5 than that at pH 7.4. The cellular uptake of CS-modified PLGA NPs increased compared with PLGA NPs, while cell viability was reduced. In conclusion, these results indicated that CS-modified, PTX-loaded PLGA NPs have the advantages of sustained drug release and enhanced drug toxicity, suggesting that CS-modified NPs can be used as carriers of anticancer drugs.

Synthesis, Characterization and in-vitro drug release studies of a macromolecular prodrug of Didanosine.

2010 ◽  
Vol 2 (2) ◽  
Author(s):  
Neeraj Agrawal ◽  
M.J. Chandrasekar ◽  
U.V. Sara ◽  
Rohini A.
Keyword(s):  
Drug Release ◽  
Drug Level ◽  
Drug Release Profile ◽  
Sustained Drug Release ◽  
In Vitro Drug Release ◽  
Alkaline Environment ◽  
Stomach Acid ◽  
Release Studies ◽  
Macromolecular Prodrug

A macromolecular prodrug of didanosine (ddI) for oral administration was synthesized and evaluated for in-vitro drug release profile. Didanosine was first coupled to 2-hydroxy ethyl methacrylate (HEMA) through a succinic spacer to form HEMA-Suc-ddI monomeric conjugate which was subsequently polymerized to yield Poly(HEMA-Suc-ddI) conjugate. The structures of the synthesized compounds were characterized by FT-IR, Mass and 1H-NMR spectroscopy. The prodrug was subjected for in-vitro drug release studies in buffers of pH 1.2 and 7.4 mimicking the upper and lower GIT. The results showed that the drug release from the polymeric backbone takes place in a sustained manner over a period of 24 h and the amount of drug released was comparatively higher at pH 7.4 indicating that the drug release takes place predominantly at the alkaline environment of the lower GIT rather than at the acidic environment of the upper GIT. This pH dependent sustained drug release behavior of the prodrug may be capable of reducing the dose limiting toxicities by maintaining the plasma drug level within the therapeutic range and increasing t1/2 of ddI. Moreover, the bioavailability of the drug should be improved as the prodrug releases ddI predominantly in the alkaline environment which will reduce the degradation of ddI in the stomach acid.

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